Ctrl

K

Abiraterone

Class
Steroidogenesis inhibitors
Subclass
Androgen biosynthesis inhibitors
Substance name
Abiraterone acetate
Brand names
Zytiga®
Common formulations
Tablet
Dosage and administration
Adults patients
Prostate cancerMetastatic, castration-sensitive
1,000 mg PO daily
Prostate cancerCastration-resistant, metastatic
1,000 mg PO daily
Prostate cancerMetastatic, castration-resistant
500 mg PO daily
Indications for use
Labeled indications
Adults
Adjunctive treatment for prostate cancer (castration-resistant, metastatic)
Adjunctive treatment for prostate cancer (metastatic, castration-resistant)
Adjunctive treatment for prostate cancer (metastatic, castration-sensitive)
Safety risks
Contraindications
Patients with pre-existing moderate or severe hepatic impairment
Warnings and precautions
Adrenal insufficiency
Use caution in patients receiving abiraterone in combination with prednisone.
Hypoglycemia
Use caution in patients who have pre-existing diabetes mellitus.
Reactivation of HF
Use caution Patients having medical conditions that may be affected by increases to BP, electrolyte abnormalities, or fluid retention.
Specific populations
Renal impairment
eGFR 20-50 mL/min/1.73 m²
Use acceptable. No dose adjustment required.
eGFR 10-20 mL/min/1.73 m²
Use acceptable. No dose adjustment required.
eGFR < 10 mL/min/1.73 m²
No dose adjustment required. Cap dose.
Renal replacement therapy
Continuous renal replacement
Use with caution.
Intermittent hemodialysis
Use with caution.
Peritoneal dialysis
Use with caution.
Hepatic impairment
Child-Pugh A (mild)
Use acceptable. No dose adjustment required. Monitor serum aminotransferases. -Monitor LFTs prior to starting therapy, every week for the first month, every 2 weeks for the next 2 months, and then monthly thereafter.
Child-Pugh B (moderate)
Reduce dose. Start at dose of 250 mg PO. Monitor serum aminotransferases. Monitor for toxicity. -Monitor closely for treatment-related adverse reactions - Monitor LFTs prior to starting therapy, every week for the first month, every 2 weeks for the next 2 months, and then monthly thereafter - If elevations in ALT/AST > 5 times ULN or total bilirubin > 3 times ULN occur, permanently discontinue abiraterone.
Child-Pugh C (severe)
Do not use.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: D
Do not use. Evidence of fetal harm in humans. Pregnancy should be avoided by female partners of men receiving therapy with abiraterone during treatment and for 1 week after the last dose.
Instruct pregnant women or females of reproductive potential to NOT handle abiraterone tablets without protection (e.g., gloves). Although there are no adequately controlled studies in pregnant women, abiraterone can cause fetal harm or death when administered during pregnancy based on its mechanism of action and animal studies.
Breastfeeding
Little information available on breastfeeding safety.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
↓ blood lymphocyte count, hypertension, ↑ serum ALP, fatigue, arthralgia, nausea, edema, hot flashes, cough, headache, diarrhea, vomiting, ↑ serum triglycerides, ↑ serum cholesterol, ↓ serum potassium, ↑ blood glucose, anemia, upper respiratory tract infections
Unknown frequency
Common cold, dizziness, confusion, ↑ HR, muscle weakness, feeling faint, lightheadedness, leg pain
Interactions
Drug(s)
Check Interactions
Reset

What did you think about this content?

Create free account

Sign up for free to access the full drug resource